Syntheses and Structure-Activity Relationships in Antibacterial Activity against Clostridium difficile and XBP1 Activation Property of 13-[(N-Alkylamino)methyl]-8-oxodihydrocoptisines
© 2020 Wiley-VHCA AG, Zurich, Switzerland..
13-[(N-Alkylamino)methyl]-8-oxodihydrocoptisines were synthesized to evaluate antibacterial activity against Clostridium difficile and activating x-box-binding protein 1 (XBP1) activity, biological properties both associated with ulcerative colitis. Improving structural stability and ameliorating biological activity were major concerns. Different substituents on the structural modification site were involved to explore the influence of diverse structures on the bioactivities. The target compounds exhibited the desired activities with definite structure-activity relationship. In the series of 13-[(N-n-alkylamino)methyl]-8-oxodihydrocoptisines, the length of n-alkyl groups has a definite effect on the bioactivity, elongation of the length increasing the antibacterial activity. The synthesized compounds were determined to display strong or weak XBP1-activating activity in vitro. The preliminary results of this study warrant further medicinal chemistry studies on these synthesized compounds.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:17 |
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| Enthalten in: |
Chemistry & biodiversity - 17(2020), 7 vom: 08. Juli, Seite e2000265 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Li, Jing [VerfasserIn] |
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| Links: |
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| Themen: |
Anti-Bacterial Agents |
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| Anmerkungen: |
Date Completed 25.05.2021 Date Revised 25.05.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1002/cbdv.202000265 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM309482518 |
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| 245 | 1 | 0 | |a Syntheses and Structure-Activity Relationships in Antibacterial Activity against Clostridium difficile and XBP1 Activation Property of 13-[(N-Alkylamino)methyl]-8-oxodihydrocoptisines |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2020 Wiley-VHCA AG, Zurich, Switzerland. | ||
| 520 | |a 13-[(N-Alkylamino)methyl]-8-oxodihydrocoptisines were synthesized to evaluate antibacterial activity against Clostridium difficile and activating x-box-binding protein 1 (XBP1) activity, biological properties both associated with ulcerative colitis. Improving structural stability and ameliorating biological activity were major concerns. Different substituents on the structural modification site were involved to explore the influence of diverse structures on the bioactivities. The target compounds exhibited the desired activities with definite structure-activity relationship. In the series of 13-[(N-n-alkylamino)methyl]-8-oxodihydrocoptisines, the length of n-alkyl groups has a definite effect on the bioactivity, elongation of the length increasing the antibacterial activity. The synthesized compounds were determined to display strong or weak XBP1-activating activity in vitro. The preliminary results of this study warrant further medicinal chemistry studies on these synthesized compounds | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a XBP1-activating activity | |
| 650 | 4 | |a antibacterial activity | |
| 650 | 4 | |a quaternary coptisine chloride | |
| 650 | 4 | |a structure modification | |
| 650 | 4 | |a structure-activity relationships | |
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| 650 | 7 | |a X-Box Binding Protein 1 |2 NLM | |
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| 700 | 1 | |a Li, Zhi-Hong |e verfasserin |4 aut | |
| 700 | 1 | |a Xing, Ya-Ling |e verfasserin |4 aut | |
| 700 | 1 | |a Wu, Lian-Qiu |e verfasserin |4 aut | |
| 700 | 1 | |a Qin, Hai-Lin |e verfasserin |4 aut | |
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